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YY2201 is a highly potent and selective small-molecule inhibitor of ATR (ataxia telangiectasia and Rad3-related protein), a key kinase in the DNA damage response pathway. By inhibiting ATR, YY2201 induces DNA damage accumulation and apoptosis, particularly in cancer cells with deficiencies or mutations in other DNA damage response kinases, exploiting synthetic lethality. Preclinical studies have demonstrated that YY2201 efficiently inhibits tumor progression across a broad spectrum of cancer types both in vitro and in vivo, showing superior anticancer efficacy compared to AZD6738 (ceralasertib) in lung cancer xenograft models. The drug has favorable pharmacokinetic properties and safety profiles, with promising activity as monotherapy or combined with chemotherapy. It is being developed primarily for the treatment of advanced solid tumors[4][5][2].
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